SEL201

SEL201 is a potent and selective small molecule inhibitor of the MAP kinase-interacting kinases 1 and 2 (MNK1/2). MNK1/2 are serine/threonine kinases that act as downstream effectors of the MAPK pathway, specifically responsible for the phosphorylation of eukaryotic initiation factor 4E (eIF4E) at Ser209. This phosphorylation is a critical step in the regulation of protein translation initiation, often exploited by cancer cells to selectively enhance the translation of oncogenic mRNAs involved in cell survival, proliferation, and metastasis. By inhibiting MNK1/2, SEL201 suppresses the MNK-eIF4E axis, thereby reducing the expression of pro-tumorigenic proteins. Research has demonstrated that SEL201 can synergize with other targeted therapies, such as BET inhibitors (e.g., OTX015), to overcome resistance in melanoma by targeting novel vulnerabilities like TGM2 and focal adhesion kinase (FAK) signaling. SEL201 was developed by Ryvu Therapeutics (formerly Selvita) as part of their oncology pipeline.

Other names

MNK1/2 inhibitor SEL201